Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine

  • Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21. doi: 10.1016/j.bmcl.2004.05.079.
Vasudha Sharma  1 ,  Jetze J Tepe
Affiliations
  • 1. Department of Chemistry, Michigan State University, East Lansing, MI 48824, USA.
PMID: 15261294 DOI: 10.1016/j.bmcl.2004.05.079
Abstract

The marine Sponge metabolite hymenialdisine is a potent inhibitor of a variety of kinases including MEK-1, GSK-3 beta, and CK1. In addition, hymenialdisine and debromohymenialdisine exhibit inhibition of the G(2) cell cycle checkpoint at micromolar concentrations. We report herein the potent inhibition of cell cycle kinase Chk2 by the indolic-hymenialdisine indoloazepine 1 (IC(50)=8 nM).

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